Reaction Derivative Quercetin, Luteolin, And Kaempferol

Flavonoids are a kind of natural compounds, which are widely distributed in nature. The contents of flavonoids are very high in natrure and their structures are diversiform. Flavonoid compounds exhibited all kinds of biological activities, including antitumor activity, antioxidant activity, anti-inflammatory activity, anti-aging activity, antibacterial and antiviral activity. Some recent studies indicated that some flavonids possessed anti-HIV activity. Therefore, flavonids are prospective in clinical medicine and health food. However, flavonoids also have some defects, for example low solubility. And their biological activities are lower than cisplatin, paclitaxel and camptothecin. These defects restrict their application. It’s necessary to improve the biological activities of flavonoids according to their structure modification.Quercetin, luteolin and kaempferol are three typical flavonoids. They have general biological activities. The most important biological activities are antitumor and anticancer activities. Althrough many researchers have reported their biological activities and structure modification, the derivatization researches of these three flavonoids are still not enough.This dissertation consists of six chapters. The derivatization and biological activities of quercetin, luteolin and kaempferol were summarized in the first chapter. The second chapter introduced the derivatization of quercetin by our experiments. Ten derivative compounds were synthesized by esterification, acylation, etherification, hydrogenation and introduction of heteroatoms. A quercetin derivative comprised a nitrogen (6’-piperidino-quercetin) was synthesized in this study. This compound showeds higher anti-HIV activity than other nature compounds isolated from plants in our group. The synthesis of derivatives of luteolin was introduced in the third chapter, and six derivatives of luteolin was synthesized. The synthesis of kaempferol derivatives was introduced in the forth chap, and six derivatives of kaempferol were synthesized. A new skeleton bisflavonyl was synthesized in the fifth chapter. According to the related literature the new skeleton bisflavonyl maybe have antibacterial and anti-inflammatory activity, especially against the golden staphylococcus bacteria. The avtivity test of this compound is ongoing. The last chapter was about the conclusion and discussion of the experiment.